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ES8704443A1 - Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, intermediates thereto, and processes. - Google Patents

Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, intermediates thereto, and processes.

Info

Publication number
ES8704443A1
ES8704443A1 ES544852A ES544852A ES8704443A1 ES 8704443 A1 ES8704443 A1 ES 8704443A1 ES 544852 A ES544852 A ES 544852A ES 544852 A ES544852 A ES 544852A ES 8704443 A1 ES8704443 A1 ES 8704443A1
Authority
ES
Spain
Prior art keywords
hydroxymorphinans
intermediates
processes
prodrug derivatives
ester prodrug
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
ES544852A
Other languages
Spanish (es)
Other versions
ES544852A0 (en
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
EIDP Inc
Original Assignee
EI Du Pont de Nemours and Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by EI Du Pont de Nemours and Co filed Critical EI Du Pont de Nemours and Co
Publication of ES544852A0 publication Critical patent/ES544852A0/en
Publication of ES8704443A1 publication Critical patent/ES8704443A1/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22—Bridged ring systems
    • C07D221/28—Morphinans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans are useful as analgesics or narcotic antagonists and provide enhanced bioavailability of 3-hydroxymorphinans from orally administered doses.
ES544852A 1984-07-05 1985-07-04 Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, intermediates thereto, and processes. Expired ES8704443A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62792384A 1984-07-05 1984-07-05
US06/733,464 US4668685A (en) 1984-07-05 1985-05-14 Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists

Publications (2)

Publication Number Publication Date
ES544852A0 ES544852A0 (en) 1987-04-01
ES8704443A1 true ES8704443A1 (en) 1987-04-01

Family

ID=27090564

Family Applications (1)

Application Number Title Priority Date Filing Date
ES544852A Expired ES8704443A1 (en) 1984-07-05 1985-07-04 Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, intermediates thereto, and processes.

Country Status (18)

Country Link
US (1) US4668685A (en)
EP (1) EP0170090B1 (en)
AU (1) AU578391B2 (en)
CA (1) CA1301150C (en)
DE (1) DE3573251D1 (en)
DK (1) DK160501C (en)
ES (1) ES8704443A1 (en)
FI (1) FI83215C (en)
GR (1) GR851653B (en)
HK (1) HK39790A (en)
HU (1) HU193995B (en)
IE (1) IE58136B1 (en)
IL (1) IL75721A (en)
MX (1) MX160445A (en)
NO (1) NO171209C (en)
NZ (1) NZ212641A (en)
PT (1) PT80773B (en)
SU (2) SU1450742A3 (en)

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DK107688D0 (en) * 1988-03-01 1988-03-01 Novo Industri As CARBAMIC ACID ESTERS OF SUBSTITUTED 7-HYDROXY-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINES
US6702705B1 (en) 1988-05-04 2004-03-09 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
DK24089D0 (en) * 1989-01-20 1989-01-20 Hans Bundgaard NOVEL PRODRUG DERIVATIVES OF BIOLOGICALLY ACTIVE AGENTS CONTAINING HYDROXYL GROUPS OR NH-ACIDIC GROUPS
US6258360B1 (en) * 1989-05-04 2001-07-10 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
JPH06510529A (en) * 1991-08-05 1994-11-24 イゲン，インコーポレーテッド Prodrugs activated by targeted catalytic proteins
US5968551A (en) * 1991-12-24 1999-10-19 Purdue Pharma L.P. Orally administrable opioid formulations having extended duration of effect
ES2121988T3 (en) * 1992-01-23 1998-12-16 Toray Industries DERIVATIVE OF MORFINANO AND MEDICINAL USE.
TW372972B (en) * 1992-10-23 1999-11-01 Novartis Ag Antiretroviral acyl compounds
EP0615756B1 (en) * 1993-03-15 2001-06-27 National Science Council Nalbuphine esters and long-acting pharmaceutical compositions containing them
DE69424853T2 (en) * 1993-07-23 2000-10-05 Toray Industries, Inc. MORPHINAN DERIVATIVES AND THEIR MEDICAL USE
US5376662A (en) * 1993-12-08 1994-12-27 Ockert; David M. Method of attenuating nerve injury induced pain
US5869669A (en) * 1996-07-26 1999-02-09 Penick Corporation Preparation of 14-hydroxynormorphinones from normorphinone dienol acylates
US6225321B1 (en) * 1997-06-05 2001-05-01 Oliver Yoa-Pu Hu Long analgesic acting nalbuphine polyester derivative and method of use
NZ505193A (en) 1997-12-22 2003-03-28 Euro Celtique S Opioid agonist/antagonist combinations
US6375957B1 (en) 1997-12-22 2002-04-23 Euro-Celtique, S.A. Opioid agonist/opioid antagonist/acetaminophen combinations
ES2188481T3 (en) * 2000-04-27 2003-07-01 Oliver Yoa-Pu Hu DERIVATIVES OF POLINALBUFINA.
US6569449B1 (en) 2000-11-13 2003-05-27 University Of Kentucky Research Foundation Transdermal delivery of opioid antagonist prodrugs
ES2361148T3 (en) 2001-05-11 2011-06-14 Endo Pharmaceuticals Inc. DOSAGE FORM OF ABUSE RESISTANT CONTROLLED OPIOID OPTION.
MXPA04001647A (en) * 2001-08-23 2004-05-31 Akzo Nobel Nv Process for the preparation of a 14-hydroxynormorphinone derivative.
US20040033253A1 (en) * 2002-02-19 2004-02-19 Ihor Shevchuk Acyl opioid antagonists
PT1492505E (en) 2002-04-05 2015-10-06 Euro Celtique Sa Pharmaceutical preparation containing oxycodone and naloxone
US20040202717A1 (en) 2003-04-08 2004-10-14 Mehta Atul M. Abuse-resistant oral dosage forms and method of use thereof
US20080020028A1 (en) * 2003-08-20 2008-01-24 Euro-Celtique S.A. Transdermal dosage form comprising an active agent and a salt and a free-base form of an adverse agent
EP1604666A1 (en) * 2004-06-08 2005-12-14 Euro-Celtique S.A. Opioids for the treatment of the Chronic Obstructive Pulmonary Disease (COPD)
EP1604667A1 (en) * 2004-06-08 2005-12-14 Euro-Celtique S.A. Opioids for the treatment of the restless leg syndrome
JP2008514612A (en) * 2004-09-23 2008-05-08 ミシャロウ、アレクサンダー Methods of modulating neurotransmitter systems by inducing counter adaptation
US20080045610A1 (en) * 2004-09-23 2008-02-21 Alexander Michalow Methods for regulating neurotransmitter systems by inducing counteradaptations
EP3228308A1 (en) * 2005-01-28 2017-10-11 Euro-Celtique S.A. Alcohol resistant dosage forms
EP1702558A1 (en) * 2005-02-28 2006-09-20 Euro-Celtique S.A. Method and device for the assessment of bowel function
EP1695700A1 (en) * 2005-02-28 2006-08-30 Euro-Celtique S.A. Dosage form containing oxycodone and naloxone
WO2006126529A1 (en) * 2005-05-25 2006-11-30 Shionogi & Co., Ltd. 6,7-unsaturated-7-carbamoyl substituted morphinan derivative
US8163701B2 (en) 2005-08-19 2012-04-24 Signature Therapeutics, Inc. Prodrugs of active agents
GB0606124D0 (en) * 2006-03-28 2006-05-03 Reckitt Benckiser Healthcare Buprenorphine derivatives and uses thereof
US8178551B2 (en) * 2007-03-09 2012-05-15 Green Cross Corporation Orally bioavailable prodrugs of (+)-3-hydroxymorphinan for Parkinson'S disease prevention or treatment
CN102143740A (en) * 2008-07-07 2011-08-03 欧洲凯尔特公司 Use of opioid antagonists to treat urinary retention
AU2010223323B2 (en) 2009-03-10 2013-07-04 Euro-Celtique S.A. Immediate release pharmaceutical compositions comprising oxycodone and naloxone
UA102916C2 (en) 2009-07-02 2013-08-27 Кемфарм, Інк. Composition based on conjugates of hydrocodone with benzoic acid, benzoic acid or heteroaryl carboxylic acid derivatives, prodrugs and method for treatment of abuses
US10849981B2 (en) 2009-07-02 2020-12-01 KemPham, Inc. Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof
US8623888B2 (en) * 2009-07-15 2014-01-07 Mallinckrodt Llc 3-oxy-hydromorphone derivatives
EP2639234B1 (en) 2010-11-12 2019-07-03 Shionogi&Co., Ltd. Crystalline 6,7-unsaturated-7-carbamoyl morphinane derivative, and method for producing same
MX362857B (en) 2011-10-26 2019-02-20 Kempharm Inc Star Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof.
EP3024461B1 (en) 2013-07-23 2020-05-13 Euro-Celtique S.A. A combination of oxycodone and naloxone for use in treating pain in patients suffering from pain and a disease resulting in intestinal dysbiosis and/or increasing the risk for intestinal bacterial translocation
JP6400848B2 (en) 2014-11-25 2018-10-03 ケムファーム・インコーポレーテッド Benzoic acid, benzoic acid derivatives and heteroarylcarboxylic acid conjugates of oxycodone
KR20170094251A (en) 2014-12-02 2017-08-17 켐팜 인코포레이티드 Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods and making and use thereof
US10155771B2 (en) * 2015-11-04 2018-12-18 Noramco, Inc. Selective reduction of morphinan alkaloids
US10807995B2 (en) 2018-07-13 2020-10-20 Alkermes Pharma Ireland Limited Thienothiophene compounds for long-acting injectable compositions and related methods
WO2020012248A1 (en) 2018-07-13 2020-01-16 Alkermes Pharma Ireland Limited Novel naphthylenyl compounds for long-acting injectable compositions and related methods
US11186585B2 (en) 2018-08-17 2021-11-30 Kappa-Pharma LLC Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates
WO2020094634A1 (en) 2018-11-05 2020-05-14 Alkermes Pharma Ireland Limited Thiophene prodrugs of naltroxene for long-acting injectable compositions and related methods
CN114828961B (en) 2019-08-11 2024-03-29 卡帕制药有限责任公司 Compositions and methods for enhancing opioid receptor binding by opioid hexadienoates and optionally substituted hexadienoates

Family Cites Families (14)

* Cited by examiner, † Cited by third party
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DE224197C (en) *
US3254088A (en) * 1961-03-14 1966-05-31 Lewenstein Morphine derivative
FR1602610A (en) * 1962-10-10 1971-01-04 10.10.62.-17.4.63. 38445-15209 thebaine derivs
US3332950A (en) * 1963-03-23 1967-07-25 Endo Lab 14-hydroxydihydronormorphinone derivatives
IL26896A (en) * 1966-01-19 1970-11-30 Endo Lab 14-hydroxynormorphines and 14-hydroxynormorphinones
GB1097167A (en) * 1966-05-31 1967-12-29 Shionogi & Co 3-hydroxy-6-oxo-n-phenethylmorphinan compounds and their production
CH543514A (en) * 1967-08-25 1973-10-31 Hoffmann La Roche Process for the preparation of morphinane derivatives
US3654280A (en) * 1968-03-21 1972-04-04 Shionogi & Co L-n allylic-3-hydroxy-6-oxomorphinans
DE2323192A1 (en) * 1972-05-10 1973-12-13 Endo Lab INJECTABLE LONG-ACTING ANTAGONIS PREPARATIONS AGAINST NARCOTICS AND DRUGS
US4161597A (en) * 1976-12-20 1979-07-17 Research Corporation N-alkyl-14-hydroxymorphinans and derivatives
JPS59184182A (en) * 1983-04-02 1984-10-19 Res Inst For Prod Dev 3-benzoylthio-4,5α-epoxy-7α-[1(R)-hydroxy-1-methylbentyl]-6-methoxy-17-methyl-6,14-endo-ethanomorphinan
JPS59184163A (en) * 1983-04-02 1984-10-19 Res Inst For Prod Dev 3-benzoylthio-17-methylmorphinan
JPS59184183A (en) * 1983-04-02 1984-10-19 Res Inst For Prod Dev 3-benzoylthio-4,5alpha-epoxy-7alpha-(1(r)-hydroxyl-1-methylbutyl)-6- methoxy-17-methyl-6,14-endo-ethenomorphinan
JPS59186987A (en) * 1983-04-06 1984-10-23 Res Inst For Prod Dev 3-benzoylthio-4,5α-epoxy-7α-[1(R)-hydroxy-1-methylbutyl]-6-methoxy-17-methyl-6,14-endo-ethenomorphinan

Also Published As

Publication number Publication date
IL75721A (en) 1990-04-29
MX160445A (en) 1990-03-02
IE851683L (en) 1986-01-05
EP0170090A1 (en) 1986-02-05
AU578391B2 (en) 1988-10-20
DK160501B (en) 1991-03-18
FI83215B (en) 1991-02-28
IL75721A0 (en) 1985-11-29
HUT40132A (en) 1986-11-28
SU1450742A3 (en) 1989-01-07
DK306885D0 (en) 1985-07-04
GR851653B (en) 1985-11-26
PT80773A (en) 1985-08-01
FI852659A0 (en) 1985-07-04
CA1301150C (en) 1992-05-19
EP0170090B1 (en) 1989-09-27
FI852659L (en) 1986-01-06
AU4451685A (en) 1986-01-09
SU1508960A3 (en) 1989-09-15
ES544852A0 (en) 1987-04-01
NO852699L (en) 1986-01-06
PT80773B (en) 1987-10-20
NO171209B (en) 1992-11-02
HU193995B (en) 1987-12-28
US4668685A (en) 1987-05-26
FI83215C (en) 1991-06-10
DK160501C (en) 1991-08-26
DE3573251D1 (en) 1989-11-02
IE58136B1 (en) 1993-07-14
NZ212641A (en) 1988-10-28
HK39790A (en) 1990-06-01
NO171209C (en) 1993-02-10
DK306885A (en) 1986-01-06

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Legal Events

Date Code Title Description
FD1A Patent lapsed

Effective date: 19970203